MK-3207|cas:957118-49-9|西域试剂

MK-3207,99.60%

产品编号：Bellancom-10301| CAS NO：957118-49-9| 分子式：C₃₁H₂₉F₂N₅O₃| 分子量：557.59

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-10301		￥1920.00	杭州北京（现货）
Bellancom-10301		￥3300.00	杭州北京（现货）

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MK-3207

产品介绍

MK-3207 是一种口服有效的、具有高选择性和种属特异性的 CGRP 受体拮抗剂 (对人 CGRP 受体：IC₅₀=0.12 nM; K_i=0.024 nM)。MK-3207 可用于偏头痛的研究。

生物活性

MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC₅₀=0.12 nM; K_i=0.024 nM). MK-3207 can be used for migraine studies.

体外研究

MK-3207 (0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM; 30 min) potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	HEK293 cells (stably expressing human CLR/RAMP1)
Concentration:	0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM
Incubation Time:	30 min (pre-treat)
Result:	Blocked human α-CGRP-stimulated cAMP responses with an IC₅₀ value of 0.12 nM.

体内研究
(In Vivo)

MK-3207 (0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg; i.v.; single) inhibits CIDV in rhesus monkeys with EC₅₀ and E_max values of approximately 0.8 nM and 81%.
MK-3207 (10 mg/kg; p.o.; single) shows the CSF/plasma ratio is 2 to 3%.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult rhesus monkeys (4.8-12.7 kg; capsaicin-induced).
Dosage:	0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg
Administration:	Intravenous injection; single.
Result:	Resulted in an exposure-dependent decrease in capsaicin-induced dermal vasodilation in the rhesus monkey forearm.

Animal Model:	Adult rhesus monkeys (4.8-12.7 kg).
Dosage:	10 mg/kg
Administration:	Oral administration; single.
Result:	Exhibited the CSF/plasma ratio was 2 to 3%, however the CSF/plasma ratio was approximately 30% of the unbound fraction (9.4%) in plasma.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult rhesus monkeys (4.8-12.7 kg; capsaicin-induced).
Dosage:	0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg
Administration:	Intravenous injection; single.
Result:	Resulted in an exposure-dependent decrease in capsaicin-induced dermal vasodilation in the rhesus monkey forearm.

Animal Model:	Adult rhesus monkeys (4.8-12.7 kg).
Dosage:	10 mg/kg
Administration:	Oral administration; single.
Result:	Exhibited the CSF/plasma ratio was 2 to 3%, however the CSF/plasma ratio was approximately 30% of the unbound fraction (9.4%) in plasma.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult rhesus monkeys (4.8-12.7 kg; capsaicin-induced).
Dosage:	0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg
Administration:	Intravenous injection; single.
Result:	Resulted in an exposure-dependent decrease in capsaicin-induced dermal vasodilation in the rhesus monkey forearm.

Animal Model:	Adult rhesus monkeys (4.8-12.7 kg).
Dosage:	10 mg/kg
Administration:	Oral administration; single.
Result:	Exhibited the CSF/plasma ratio was 2 to 3%, however the CSF/plasma ratio was approximately 30% of the unbound fraction (9.4%) in plasma.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 150 mg/mL (269.01 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7934 mL	8.9672 mL	17.9343 mL
5 mM	0.3587 mL	1.7934 mL	3.5869 mL
10 mM	0.1793 mL	0.8967 mL	1.7934 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。